Synthesis and receptor binding of thiophene bioisosteres of potent GluN2B ligands with a benzo[7]annulene-scaffold
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Med. Chem. Commun., 2019, Advance Article
DOI: 10.1039/C8MD00545A, Research Article
Sören Baumeister, Dirk Schepmann, Bernhard Wünsch
Bioisosteric [7]annulenothiophenes are well tolerated by GluN2B subunit containing NMDA receptors, but do not require a benzylic OH moiety.
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Identification of the first enantiopure Rac1–Tiam1 protein–protein interaction inhibitor and its optimized synthesis via phosphine free remote group directed hydroarylation
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Med. Chem. Commun., 2019, Advance Article
DOI: 10.1039/C8MD00477C, Research Article
Alessandro Ruffoni, Nicola Ferri, Andrea Pinto, Sara Pellegrino, Alessandro Contini, Francesca Clerici
The remote substituent regiocontrol of phosphine free Heck hydroarylation has been exploited for the preparation of the first enantiopure inhibitor of Rac1–Tiam1 PPI.
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Isatin and its derivatives: A survey of recent syntheses, reactions, and applications.
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Med. Chem. Commun., 2019, Accepted Manuscript
DOI: 10.1039/C8MD00585K, Review Article
Varun Chahal, SONAM NIRWAN, Rita Kakkar
Isatin (1H-indole-2,3-dione) and its derivatives represent an important class of heterocyclic compounds that can be used as precursors for drug synthesis. Since its discovery, a lot of research
work has...
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‘Second-generation’ 1,2,3-triazole-based inhibitors of Porphyromonas gingivalis adherence to oral streptococci and biofilm formation
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Med. Chem. Commun., 2019, Advance Article
DOI: 10.1039/C8MD00405F, Research Article
Open Access
This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Pravin C. Patil, Jinlian Tan, Donald R. Demuth, Frederick A. Luzzio
This study details the design, synthesis and bioassay of ‘click’ peptidomimetic compounds which inhibit the adherence of P. gingivalis to S. gordonii, a primary step toward
pathogenic colonization of the subgingival pocket.
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Design and characterization of a heterocyclic electrophilic fragment library for the discovery of cysteine-targeted covalent inhibitors
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Med. Chem. Commun., 2019, Advance Article
DOI: 10.1039/C8MD00327K, Research Article
A. Keeley, P. Ábrányi-Balogh, G. M. Keserű
A fragment library of electrophilic small heterocycles was characterized through cysteine-reactivity and aqueous stability tests that suggested their potential as covalent warheads.
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Prospective treatment of Parkinson's disease by a siRNA–LDH nanoconjugate
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Med. Chem. Commun., 2019, Advance Article
DOI: 10.1039/C8MD00501J, Research Article
Rituparna Acharya, Monisha Chakraborty, Jui Chakraborty
51.55% cellular internalization of an α-syn siRNA–LDH nanoconjugate was corroborated through confocal imaging.
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Progress toward allosteric ligands of metabotropic glutamate 7 (mGlu7) receptor: 2008–present
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Med. Chem. Commun., 2019, Advance Article
DOI: 10.1039/C8MD00524A, Review Article
Henar Vázquez-Villa, Andrés A. Trabanco
Metabotropic glutamate type 7 (mGlu7) receptor is a member of the group III family of mGlu receptors.
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Efforts in redesigning the antileukemic drug 6-thiopurine: decreasing toxic side effects while maintaining efficacy
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Med. Chem. Commun., 2019, Advance Article
DOI: 10.1039/C8MD00463C, Research Article
Arnaldo X. Torres Hernandez, Chamitha J. Weeramange, Prathibha Desman, Anthony Fatino, Olivia Haney, Ryan J. Rafferty
Investigations into the mode of toxicity of 6-thiopurine has led to the construction of three new analogs that retain efficacy with decreased toxicity.
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Recent developments in compounds acting in the DNA minor groove
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Med. Chem. Commun., 2019, Advance Article
DOI: 10.1039/C8MD00425K, Review Article
Adeyemi Rahman, Patrick O'Sullivan, Isabel Rozas
DNA minor groove is the target: the small molecules' attack.
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